水飞蓟宾在不同介质中平衡溶解度和表观油水分配系数的测定_张婷婷.pdfVIP

* 张婷婷, 徐文, 胡生亮, 何仲贵 , 110016 : 测定水飞蓟宾在水和表面活性剂溶液中的平衡溶解度 及在正辛醇- 水/ 缓冲液体系中的表观油水分配系数 采用高效液相法测定了水飞蓟宾在水缓冲液和表面活性剂溶液中的浓度, 采用摇瓶法测定了水飞蓟宾的表观油水分配 系数 3 e 水飞蓟宾在水中的平衡溶解度为51106 mg#L- 1, 在碱性缓冲液中溶解度增大; 聚山梨酯80 和泊洛沙姆 188 对水飞蓟宾有较强的增溶能力; 水飞蓟宾的表观油水分配系数为 98910 水飞蓟宾的水溶性较差, 提高其口服制剂的 溶出度可能会提高其生物利用度 : 水飞蓟宾; 平衡溶解度; 表观油水分配系数; 高效液相色谱法 : R943141 :A : 1001- 2494 2006 20- 1569- 03 Determination of Equilibrium Solubility of Silibinin in Various Medium and Its Apparent Oil/ Water Partition Coefficient * ZHANG Ting-ting, XU Wen, HU Sheng-liang, HE Zhong-gui Department of Pharmaceutics, Shenyang Pharmaceutical Universi- ty, Sheny ang 110016, China ABS RAC : OBJEC IVE To determine the equilibrium solubility of silibinin in various surfactant solutions and its partition coefficients for the n-octano-l water/ buffer solution systems1 ME HODS A high performance liquid chromatography methodwas established and used to de- tect the concentration of silibinin in water, buffer solutions and surfactant solutions; the partition coefficients for the n-octano-l water/ buffer so- lution systems of silibinin were determined by shaking flask method1 RESUL S The equilibrium solubility of silibinin in water was 51106 mg#L- 1 at 3 e and had higher values in basic buffer solutions; polysorbate 80 and poloxamer 188 were good solubilizers for silibinin; P of app silibinin was 989101 CONCLUSION Silibinin is a hydrophobic drug; increasing the dissolution rate of silibinin from its oral drug delivery system may have the possibility to enhance its bioavailability1 KEY WORDS:silibinin; equilibrium solubility; apparent oil/ water partition coefficient; HPLC silymarin, SL [Silybum marianum L1 Gaertn1] , silibinin, SLB , A 1 水飞蓟宾结构式 B, 1 1- A;2- B , , , Fig 1 Structure of silibinin 1- silibinin A; 2- silibinin B [ 1] , , ; PHS- 2C LDZ5- 2 , 座机电话号码, 31%, ; 1 ; 80 JASCO PU - 2080 Plus intelli- ; 400 , gent HPLC Pump, UV - 20 5 Plus intelligent UV/ VIS 座机电话号码 ; 188 , Detector, JASC